EP4245369A3 - Neuroactive steroids, compositions, and uses thereof - Google Patents

Neuroactive steroids, compositions, and uses thereof Download PDF

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Publication number
EP4245369A3
EP4245369A3 EP23171488.2A EP23171488A EP4245369A3 EP 4245369 A3 EP4245369 A3 EP 4245369A3 EP 23171488 A EP23171488 A EP 23171488A EP 4245369 A3 EP4245369 A3 EP 4245369A3
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EP
European Patent Office
Prior art keywords
compositions
neuroactive steroids
compounds
formula
cns
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP23171488.2A
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German (de)
French (fr)
Other versions
EP4245369A2 (en
Inventor
Ravindra B. Upasani
Boyd L. Harrison
Benny C. ASKEW Jr
Jean-Cosme DODART
Francesco G Salituro
Albert J Robichaud
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Sage Therapeutics Inc
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Sage Therapeutics Inc
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Publication of EP4245369A2 publication Critical patent/EP4245369A2/en
Publication of EP4245369A3 publication Critical patent/EP4245369A3/en
Pending legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • C07J1/0022—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0029—Ethers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/003—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring the S atom directly linked to a ring carbon atom of the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C07J41/0011—Unsubstituted amino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/0065—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by an OH group free esterified or etherified
    • C07J7/007—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by an OH group free esterified or etherified not substituted in position 17 alfa
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J75/00—Processes for the preparation of steroids in general
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Compounds are provided according to Formula (I):
Figure imga0001
 and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v):
Figure imga0002
Figure imga0003
 and wherein L1, L2, L3, X1, X2, Y, RZ4, RZ5, RZ6, n, R1, R2, R3a, R3b, R4a, R4b, R6a, R6b, R7a, R7b, R11a, R11b, R14, R17, R19, R20, R23a, R23b, and R24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.
EP23171488.2A 2011-09-08 2012-09-07 Neuroactive steroids, compositions, and uses thereof Pending EP4245369A3 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161532427P 2011-09-08 2011-09-08
PCT/US2012/054261 WO2013036835A1 (en) 2011-09-08 2012-09-07 Neuroactive steroids, compositions, and uses thereof
EP12766766.5A EP2753632B1 (en) 2011-09-08 2012-09-07 Neuroactive steroids, compositions, and uses thereof

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EP4245369A2 EP4245369A2 (en) 2023-09-20
EP4245369A3 true EP4245369A3 (en) 2023-11-22

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EP12766766.5A Active EP2753632B1 (en) 2011-09-08 2012-09-07 Neuroactive steroids, compositions, and uses thereof

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US (4) US20150158903A1 (en)
EP (2) EP4245369A3 (en)
JP (5) JP6205362B2 (en)
CN (3) CN107936076B (en)
AU (5) AU2012304412A1 (en)
BR (1) BR112014005373B1 (en)
CA (1) CA2848212C (en)
DK (1) DK2753632T3 (en)
ES (1) ES2951664T3 (en)
FI (1) FI2753632T3 (en)
HK (1) HK1200173A1 (en)
HR (1) HRP20230747T1 (en)
HU (1) HUE062616T2 (en)
LT (1) LT2753632T (en)
PL (1) PL2753632T3 (en)
PT (1) PT2753632T (en)
RS (1) RS64332B1 (en)
RU (1) RU2665571C2 (en)
SI (1) SI2753632T1 (en)
WO (1) WO2013036835A1 (en)

Families Citing this family (75)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006047022A1 (en) 2004-10-25 2006-05-04 Virginia Commonwealth University Nuclear sulfated oxysterol, potent regulator of cholesterol homeostasis, for therapy of hypercholesterolemia, hyperlipidemia, and atherosclerosis
KR101405545B1 (en) 2005-11-28 2014-07-03 마리누스 파마슈티컬스 Ganaxolone formulations and methods for the making and use thereof
US9034859B2 (en) 2011-04-06 2015-05-19 Virginia Commonwealth University Sulfated oxysterol and oxysterol sulfation by hydroxysterol sulfotransferase promote lipid homeostasis and liver proliferation
DK2753632T3 (en) * 2011-09-08 2023-07-10 Sage Therapeutics Inc NEUROACTIVE STEROIDS, COMPOSITIONS AND USE THEREOF
US10478505B2 (en) 2011-09-23 2019-11-19 The Regents Of The University Of California Edible oils to enhance delivery of orally administered steroids
WO2013056181A1 (en) 2011-10-14 2013-04-18 Sage Therapeutics, Inc. 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof
RS59734B1 (en) 2012-01-23 2020-02-28 Sage Therapeutics Inc Neuroactive steroid formulations comprising a complex of allopregnanolone and sulfobutyl ether beta-cyclodextrin
WO2014028398A2 (en) 2012-08-13 2014-02-20 The Regents Of The University Of California Mitigation of epileptic seizures by combination therapy using benzodiazepines and neurosteroids
US20140057885A1 (en) 2012-08-21 2014-02-27 Sage Therapeutics, Inc. Methods of treating epilepsy or status epilepticus
US20150313915A1 (en) 2012-11-30 2015-11-05 The Regents Of The University Of California Anticonvulsant activity of steroids
TR201817995T4 (en) * 2013-03-13 2019-02-21 Sage Therapeutics Inc NEUROACTIVE STEROIDS AND METHODS OF USE
MX2015012437A (en) * 2013-03-13 2016-04-15 Sage Therapeutics Inc Neuroactive steroids, compositions, and uses thereof.
WO2014169836A1 (en) * 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor neuroactive steroids and methods of use thereof
CN118754924A (en) * 2013-04-17 2024-10-11 萨奇治疗股份有限公司 19-NorC 3, 3-disubstituted C21-N-pyrazolyl steroids and methods of use thereof
JP6239091B2 (en) 2013-04-17 2017-11-29 セージ セラピューティクス， インコーポレイテッド 19-nor neurostimulatory steroids and methods of use thereof
WO2014169831A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor c3,3-disubstituted c21-c-bound heteroaryl steroids and methods of use thereof
CN103333216A (en) * 2013-06-04 2013-10-02 苏州大学 5alpha-6-ketone-cholestane analogue and applications thereof
DK3021852T3 (en) 2013-07-19 2021-03-15 Sage Therapeutics Inc NEUROACTIVE STEROIDS, COMPOSITIONS AND USES
ES2706180T3 (en) 2013-08-23 2019-03-27 Sage Therapeutics Inc Neuroactive steroids, compositions and uses thereof
KR102530119B1 (en) 2013-12-24 2023-05-08 버지니아 커먼웰스 유니버시티 Uses of oxygenated cholesterol sulfates (ocs)
EP4306114A1 (en) * 2014-06-18 2024-01-17 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
US10246482B2 (en) 2014-06-18 2019-04-02 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
JOP20200195A1 (en) 2014-09-08 2017-06-16 Sage Therapeutics Inc Neuroactive steroids, compositions, and uses thereof
PE20170907A1 (en) * 2014-10-07 2017-07-12 Sage Therapeutics Inc NEUROACTIVE COMPOUNDS AND METHODS OF USING THEM
LT3206493T (en) 2014-10-16 2020-08-25 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
CN118344424A (en) 2014-10-16 2024-07-16 萨奇治疗股份有限公司 Compositions and methods for targeting CNS disorders
PT3224269T (en) 2014-11-27 2020-06-01 Sage Therapeutics Inc Compositions and methods for treating cns disorders
SI3250210T1 (en) 2015-01-26 2021-07-30 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
ES2935476T3 (en) 2015-02-20 2023-03-07 Sage Therapeutics Inc Neuroactive steroids, compositions and uses thereof
KR20240137111A (en) * 2015-07-06 2024-09-19 세이지 테라퓨틱스, 인크. Oxysterols and methods of use thereof
CA2991311A1 (en) * 2015-07-06 2017-01-12 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
IL282048B2 (en) 2015-07-06 2024-09-01 Sage Therapeutics Inc Oxysterols and methods of use thereof
BR112018001869A2 (en) * 2015-07-30 2018-09-18 Intercept Pharmaceuticals Inc method for the preparation of bile acids and derivatives thereof
HUE057613T2 (en) 2015-09-17 2022-05-28 Modernatx Inc Compounds and compositions for intracellular delivery of therapeutic agents
AU2016338672A1 (en) 2015-10-16 2018-04-12 Marinus Pharmaceuticals, Inc. Injectable neurosteroid formulations containing nanoparticles
US9637514B1 (en) 2015-10-26 2017-05-02 MAX BioPharma, Inc. Oxysterols and hedgehog signaling
US10799463B2 (en) 2015-12-22 2020-10-13 Modernatx, Inc. Compounds and compositions for intracellular delivery of agents
EP3423465A1 (en) * 2016-03-02 2019-01-09 Patheon Austria GmbH & Co KG Process and intermediates for the production of 17(20)-ene b-seco steroids
RU2766155C2 (en) 2016-03-08 2022-02-08 Сейдж Терапьютикс, Инк. Neuroactive steroids, compositions and applications thereof
CN109195604B (en) * 2016-04-01 2023-11-14 萨奇治疗股份有限公司 Oxysterol and methods of use thereof
WO2017193046A1 (en) * 2016-05-06 2017-11-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
MD3481846T2 (en) * 2016-07-07 2021-11-30 Sage Therapeutics Inc 11-substituted 24-hydroxysterols for use in the treatment of NMDA related conditions
US20190233465A1 (en) 2016-07-11 2019-08-01 Sage Therapeutics, Inc. C7, c12, and c16 substituted neuroactive steroids and their methods of use
CN109689673B (en) 2016-07-11 2023-03-14 萨奇治疗股份有限公司 C17, C20 and C21 substituted neuroactive steroids and methods of use thereof
DK3494125T3 (en) 2016-08-02 2022-08-01 Univ Virginia Commonwealth Compositions comprising 5-cholestene-3, 25-diol, 3-sulfate (25HC3S) or pharmaceutically acceptable salt thereof and at least one cyclic oligosaccharide
EP3481387A4 (en) 2016-08-11 2020-04-08 Ovid Therapeutics Inc Methods and compositions for treatment of epileptic disorders
US10391105B2 (en) 2016-09-09 2019-08-27 Marinus Pharmaceuticals Inc. Methods of treating certain depressive disorders and delirium tremens
CN110023323A (en) 2016-09-30 2019-07-16 萨奇治疗股份有限公司 The oxygen sterol that C7 replaces and its method as NMDA regulator
ES2952106T3 (en) * 2016-10-18 2023-10-27 Sage Therapeutics Inc Oxysterols and procedures for their use
BR112019008069A2 (en) * 2016-10-18 2019-09-03 Sage Therapeutics Inc oxyesterols and methods of use thereof
WO2018089540A1 (en) 2016-11-08 2018-05-17 Modernatx, Inc. Stabilized formulations of lipid nanoparticles
WO2018170336A1 (en) 2017-03-15 2018-09-20 Modernatx, Inc. Lipid nanoparticle formulation
DK3596042T3 (en) 2017-03-15 2022-04-11 Modernatx Inc CRYSTAL FORMS OF AMINOLIPIDS
HRP20230063T1 (en) 2017-03-15 2023-03-17 Modernatx, Inc. Compound and compositions for intracellular delivery of therapeutic agents
WO2018232120A1 (en) 2017-06-14 2018-12-20 Modernatx, Inc. Compounds and compositions for intracellular delivery of agents
CN109280069B (en) * 2017-07-19 2020-09-04 青岛海洋生物医药研究院股份有限公司 3 beta-hydroxy-ergosta-5-ene steroid derivative and pharmaceutical use thereof
WO2019025250A1 (en) 2017-08-04 2019-02-07 Basf Se Substituted trifluoromethyloxadiazoles for combating phytopathogenic fungi
IT201700100483A1 (en) * 2017-09-07 2019-03-07 Dipharma Francis Srl SELECTIVE OXIDATION OF IODESEXICOLIC ACID
WO2020028552A1 (en) * 2018-07-31 2020-02-06 The Research Foundation For The State University Of New York Methods of activating microglial cells
WO2020061332A1 (en) * 2018-09-19 2020-03-26 Modernatx, Inc. Sterol analogs and uses thereof
WO2020118142A1 (en) 2018-12-07 2020-06-11 Marinus Pharmaceuticals, Inc. Ganaxolone for use in prophylaxis and treatment of pospartum depression
CN115651054B (en) 2019-01-08 2024-06-21 成都康弘药业集团股份有限公司 Steroid compound, application and preparation method thereof
EP3976628A1 (en) 2019-05-31 2022-04-06 Sage Therapeutics, Inc. Neuroactive steroids and compositions thereof
JP2022543837A (en) 2019-08-05 2022-10-14 マリナス ファーマシューティカルズ， インコーポレイテッド Ganaxolone for use in treating status epilepticus
TW202124360A (en) 2019-09-19 2021-07-01 美商現代公司 Branched tail lipid compounds and compositions for intracellular delivery of therapeutic agents
US10857163B1 (en) 2019-09-30 2020-12-08 Athenen Therapeutics, Inc. Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof
WO2021113834A1 (en) 2019-12-06 2021-06-10 Marinus Pharmaceuticals, Inc. Ganaxolone for use in treating tuberous sclerosis complex
CN113387991B (en) * 2020-03-13 2024-06-18 苏州朗科生物技术股份有限公司 Method for synthesizing dydrogesterone and compound
CZ309819B6 (en) * 2020-10-23 2023-11-08 Univerzita Palackého v Olomouci Sterol derivatives, preparations containing these derivatives and their use
CN112679571A (en) * 2020-12-24 2021-04-20 广西壮族自治区中国科学院广西植物研究所 Mogrol derivative monomer, and preparation method and application thereof
JP2024520805A (en) 2021-06-11 2024-05-24 セージ セラピューティクス， インコーポレイテッド Neuroactive steroids for the treatment of Alzheimer's disease
WO2023049295A1 (en) 2021-09-22 2023-03-30 Sage Therapeutics, Inc. Deuterated positive nmda-modulating compounds and methods of use thereof
EP4447953A1 (en) 2021-12-13 2024-10-23 Sage Therapeutics, Inc. Combination of muscarinic receptor positive modulators and nmda positive allosteric modulators
CN115624555A (en) * 2022-02-24 2023-01-20 中国药科大学 Application of hyodeoxycholic acid in preparation of antidepressant drug
WO2024112759A1 (en) * 2022-11-21 2024-05-30 Sage Therapeutics, Inc. Negative nmda-modulating compounds and methods of use thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3079385A (en) * 1961-01-24 1963-02-26 Roussel Uclaf Novel process of preparation of polyhydroxylated pregnanes
JPH08268917A (en) * 1995-03-31 1996-10-15 D D S Kenkyusho:Kk Antitumor agent having high transition to cancer tissue
FR2850023A1 (en) * 2003-01-17 2004-07-23 Mapreg Treating acute lesions or degenerative diseases of the nervous system, e.g. Alzheimer's disease, spinal-cerebral trauma or pain, using 3-methoxypregnenolone or derivatives having microtubule stabilizing action

Family Cites Families (119)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2259698A (en) 1938-05-07 1941-10-21 Rare Chemicals Inc Physiologically effective substance and process of preparing same
US2594323A (en) * 1948-07-22 1952-04-29 Upjohn Co 24-substituted delta 5-cholene-3, 24-diols
US2673206A (en) 1950-06-07 1954-03-23 Schering Corp 25-ethinyl steroids
US3206459A (en) 1962-10-19 1965-09-14 Syntex Corp 10alpha-pregnan-19-ol derivatives
GB1120870A (en) 1966-07-11 1968-07-24 Ici Ltd Quinoline derivatives
JPS5248765Y2 (en) 1974-05-07 1977-11-07
US4071625A (en) 1974-05-13 1978-01-31 Richardson-Merrell Inc. 19-Oxygenated-5α-androstanes for the enhancement of libido
JPS5735597Y2 (en) 1974-05-13 1982-08-06
CH628907A5 (en) 1975-10-10 1982-03-31 Hoffmann La Roche Process for the preparation of 24,25-dihydroxycholesterol derivatives
JPS5382766U (en) 1976-12-11 1978-07-08
US4183852A (en) 1977-07-18 1980-01-15 Kaiser Emil T Process for preparing 25-hydroxycholesterol
JPS5758506Y2 (en) 1978-05-09 1982-12-14
US4174345A (en) 1978-08-01 1979-11-13 Kaiser Emil T Synthesis of steroids
US4269777A (en) 1979-05-21 1981-05-26 Wisconsin Alumni Research Foundation Isotopically labeled vitamin D derivatives and processes for preparing same
JPS61254599A (en) 1985-05-07 1986-11-12 Sumitomo Pharmaceut Co Ltd Fluorine derivative of cholesterol
JPS6253960A (en) 1985-05-30 1987-03-09 Taisho Pharmaceut Co Ltd Vitamin d3 derivative
JPS62187485U (en) 1986-05-15 1987-11-28
US5232917A (en) 1987-08-25 1993-08-03 University Of Southern California Methods, compositions, and compounds for allosteric modulation of the GABA receptor by members of the androstane and pregnane series
WO1989002272A1 (en) 1987-08-25 1989-03-23 Gee Kelvin W Compositions and methods for alleviating stress, anxiety and seizure activity
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
EP0701444B1 (en) 1993-05-24 2010-04-07 Purdue Pharma Ltd. Methods and compositions for inducing sleep
IL110309A0 (en) * 1993-07-15 1994-10-21 Univ Kentucky Res Found A method of protecting against neuron loss
DE4338316A1 (en) 1993-11-10 1995-05-11 Jenapharm Gmbh New steroids with radicallyophilic substituents, process for their preparation and medicaments containing these compounds
ATE375993T1 (en) 1994-02-14 2007-11-15 Euro Celtique Sa ANDROSTANES AND PREGANES FOR ALLOSTERIC MODULATION OF THE GABA RECEPTOR
TW385308B (en) 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
US5595996A (en) 1994-10-25 1997-01-21 Merck & Co., Inc. 7-substituted 4-aza cholanic acid derivatives and their use
DE69519945T2 (en) * 1994-11-23 2001-06-07 Cocensys, Inc. ANDROSTAN AND PREGNANSERIES FOR THE ALLOSTERIC MODULATION OF THE GABA RECEPTOR
ES2235187T3 (en) 1995-06-06 2005-07-01 Euro-Celtique S.A. NEUROACTIVE STEROIDS OF THE ANDROSTAN AND PREGNAN SERIES.
US5792635A (en) 1995-06-07 1998-08-11 Magainin Pharmaceuticals, Inc. Method of inhibiting the sodium/proton exchanger NHE3 and method of inhibiting growth by administering squalamine
CN1191543A (en) 1995-06-23 1998-08-26 诺沃挪第克公司 Meiosis regulating compounds
US6645953B2 (en) 1995-06-23 2003-11-11 Novo Nordisk A/S Meiosis regulating compounds
JP4313435B2 (en) 1995-07-24 2009-08-12 トラスティーズ オブ ボストン ユニバーシティー Inhibition of NMDA receptor activity by pregnenolone sulfate derivatives
US5888996A (en) 1995-07-26 1999-03-30 Trustees Of Boston University Inhibition of NMDA receptor activity and modulation of glutamate-mediated synaptic activity
AU3068497A (en) 1996-05-06 1997-11-26 Bionumerik Pharmaceuticals, Inc. Process for preparing 27-hydroxy cholesterol and related derivatives
JPH09328498A (en) 1996-06-10 1997-12-22 Teijin Ltd Production of 24,25-dihydroxycholesterol and its synthetic intermediate
WO1998005337A1 (en) * 1996-08-01 1998-02-12 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
DE19635525A1 (en) 1996-08-20 1998-02-26 Schering Ag New 7-alpha-(xi-aminoalkyl)- oestratriene derivatives
US6122371A (en) 1997-07-22 2000-09-19 Atwell; Ronald C. Apparatus for protecting coin-operated telephones from vandalism and larceny
EP1077933A1 (en) 1998-05-11 2001-02-28 Novo Nordisk A/S Substituted guanidines and diaminonitroethenes, their preparation and use
KR20010043558A (en) 1998-05-13 2001-05-25 한센 핀 베네드, 안네 제헤르, 웨이콥 마리안느 Meiosis regulating compounds
US8541600B2 (en) 1998-11-24 2013-09-24 Harbor Therapeutics, Inc. 11-aza, 11-thia and 11-oxa sterol compounds and compositions
DE19917930A1 (en) 1999-04-15 2000-10-19 Schering Ag Treating estrogen deficiency associated disorders, e.g. menopausal problems, osteoporosis, neoplasia or neurodegenerative disease, using new or known ent-steroids having bone-selective estrogenic activity
RU2243232C2 (en) 1999-04-29 2004-12-27 Еро-Сельтик С.А. 3alpha-hydroxy-3beta-methoxymethyl-21-heterocycle-substituted steroids, pharmaceutical composition, method for relief or prophylaxis of insomnia or narcotizing
GB9910934D0 (en) 1999-05-11 1999-07-14 Res Inst Medicine Chem Chemical compounds
GB0000228D0 (en) 2000-01-06 2000-03-01 Phytopharm Plc Fluoro substituted sapogenins and their use
DE10034222A1 (en) 2000-07-13 2002-01-31 Bosch Gmbh Robert Method and device for stabilizing a road vehicle
GB0019290D0 (en) 2000-08-04 2000-09-27 Symphar Sa Methods for inducing apolipoprotein E secretion
GR1003861B (en) 2000-12-29 2002-04-11 Novel gabaa modulating neurosteroids
GB0107822D0 (en) 2001-03-28 2001-05-23 Phytopharm Plc Sapogenin derivatives their synthesis and use methods based upon their use
US20070197484A1 (en) 2001-05-03 2007-08-23 Ching Song Method of treating disorder related to high cholesterol concentration
CA2446314C (en) 2001-05-03 2011-02-22 The University Of Chicago Liver x receptor agonists
WO2003039480A2 (en) 2001-11-08 2003-05-15 The University Of Chicago Method of treating disorder related to high cholesterol concentration
AU2002360489A1 (en) 2001-12-07 2003-06-23 The Regents Of The University Of California Treatment for age-related macular degeneration
PE20040306A1 (en) 2002-03-27 2004-05-29 Phytopharm Plc THERAPEUTIC METHODS OF SAPOGENINS AND THEIR DERIVATIVES
KR101130212B1 (en) 2002-03-27 2012-04-13 파이토팜 피엘씨 Theraputic methods and uses of SAPOGENIN and their derivatives
JP2004012949A (en) 2002-06-10 2004-01-15 Canon Inc Electrophoresis display device
US6933312B2 (en) 2002-10-07 2005-08-23 Agouron Pharmaceuticals, Inc. Pyrazole derivatives
AU2003288231A1 (en) 2002-12-13 2004-07-09 Bayer Healthcare Ag Cholesterol 24-hydroxylase (cyp46) as therapeutic target for the treatment of alzheimer's disease
GB0403889D0 (en) 2004-02-21 2004-03-24 Univ Edinburgh Uses of er-beta modulators
WO2006037016A2 (en) 2004-09-27 2006-04-06 The Regents Of The University Of California Novel therapy for treatment of chronic degenerative brain diseases and nervous system injury
US20070032464A1 (en) 2004-10-08 2007-02-08 Shutsung Liao Methods of treating cancers
JP2008518935A (en) 2004-11-01 2008-06-05 セオ ホン ユー Methods and compositions for reducing neurodegeneration in amyotrophic lateral sclerosis
US9670244B2 (en) 2006-02-27 2017-06-06 The Regents Of The University Of California Oxysterol compounds and the hedgehog pathway
ES2389743T3 (en) * 2006-04-22 2012-10-31 Harbor Biosciences, Inc. Medications and uses
CN101164540A (en) 2006-08-03 2008-04-23 中山大学 Application of marine steroids compound in preparing medicine for treating neuronal damage
GB0619860D0 (en) * 2006-10-06 2006-11-15 Birkeland Innovasjon As Treatment of insulin resistance and disorders associated therewith
US8273747B2 (en) 2006-11-02 2012-09-25 Curis, Inc. Small organic molecule regulators of cell proliferation
HUE026961T2 (en) 2006-11-21 2016-07-28 Umecrine Cognition Ab The use of pregnane and androstane steroids for the manufacture of a pharmaceutical composition for the treatment of cns disorders
WO2009073186A1 (en) 2007-12-03 2009-06-11 The Regents Of The University Of California Oxsterols for activation of hedgehog signaling, osteoinduction, antiadipogenesis, and wnt signaling
JP5587184B2 (en) 2007-06-20 2014-09-10 オースペックス・ファーマシューティカルズ・インコーポレイテッド Substituted N-arylpyridinones as fibrosis inhibitors
GB0712494D0 (en) 2007-06-27 2007-08-08 Isis Innovation Substrate reduction therapy
WO2009059239A2 (en) * 2007-11-02 2009-05-07 Mayo Foundation For Medical Education And Research REDUCING Aβ42 LEVELS AND Aβ AGGREGATION
JP2011502974A (en) 2007-11-06 2011-01-27 ナームローゼ・フエンノートチヤツプ・オルガノン Methods of hormone suppression in humans
WO2009090063A1 (en) 2008-01-16 2009-07-23 Jado Technologies Gmbh Steroid sapogenin, androstane and triterpenoid sapogenin derivatives for the treatment and prevention of infectious diseases
CA2711487A1 (en) 2008-01-25 2009-07-30 Merck Sharp & Dohme Corp. Quinolizidinone m1 receptor positive allosteric modulators
SG195568A1 (en) 2008-05-09 2013-12-30 Univ Emory Nmda receptor antagonists for the treatment of neuropsychiatric disorders
WO2010065709A2 (en) 2008-12-03 2010-06-10 Amin Khan Hydroxamic acid derivatives, preparation and therapeutic uses thereof
US20120040916A1 (en) 2008-12-22 2012-02-16 Massachusetts Institute Of Technology Molecular inhibitors of the wnt/beta-catenin pathway
US8822462B2 (en) 2009-01-28 2014-09-02 Emory University Subunit selective NMDA receptor potentiators for the treatment of neurological conditions
JP2013500986A (en) 2009-07-29 2013-01-10 ザ・ユニバーシティ・オブ・シカゴ Liver X receptor agonist
WO2011028794A2 (en) 2009-09-01 2011-03-10 Lazarus Therapeutics, Inc. Treatment of huntington's disease with cycloserine and an nmda receptor antagonist
FR2953138B1 (en) 2009-12-02 2015-10-16 Assist Publ Hopitaux Marseille AMINOSTEROIDAL COMPOUNDS FOR LOCAL TOPICAL APPLICATION FOR CUTANEO-MUCOUS DECOLONIZATION OF STAPHYLOCOCCUS AUREUS
WO2011092127A1 (en) 2010-01-26 2011-08-04 Bayer Schering Pharma Aktiengesellschaft 14,17-bridged estratriene derivatives comprising heterocyclic bioisosteres for the phenolic a-ring
KR101692275B1 (en) 2010-02-11 2017-01-04 노오쓰웨스턴 유니버시티 Secondary structure stabilized nmda receptor modulators and uses thereof
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
US20120035156A1 (en) 2010-08-09 2012-02-09 Daniela Alberati Combination of glyt1 compound with antipsychotics
US8969525B2 (en) 2010-11-09 2015-03-03 Enzo Life Sciences, Inc. Hydroxycholesterol immunoassay
WO2012142039A1 (en) 2011-04-15 2012-10-18 University Of North Dakota Combination of liver x receptor modulator and estrogen receptor modulator for the treatment of age-related diseases
CA2874998A1 (en) 2011-05-27 2012-12-06 Cytocure Llc Methods, compositions, and kits for the treatment of cancer
CA2843436A1 (en) 2011-07-29 2013-02-07 The Regents Of The University Of California Novel 17.beta.-heteroaryl-substituted steroids as modulators of gaba a receptors
DK2753632T3 (en) 2011-09-08 2023-07-10 Sage Therapeutics Inc NEUROACTIVE STEROIDS, COMPOSITIONS AND USE THEREOF
WO2013056181A1 (en) 2011-10-14 2013-04-18 Sage Therapeutics, Inc. 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof
WO2013163455A2 (en) 2012-04-25 2013-10-31 The Regents Of The University Of California A drug screening platform for rett syndrome
WO2014025942A1 (en) 2012-08-09 2014-02-13 Emory University Nmda receptor modulators and uses related thereto
US20140149272A1 (en) 2012-08-17 2014-05-29 Trueex Group Llc Interoffice bank offered rate financial product and implementation
EP4086270A1 (en) 2012-12-18 2022-11-09 Washington University Neuroactive 19-alkoxy-17-substituted steroids, useful in methods of treatment
EP3309166A3 (en) 2013-01-23 2018-08-22 Sphaera Pharma Pvt. Ltd. 11beta-hydroxy-steroids for use in mitochondria biogenesis and diseases associated with mitochondrial dysfunction or depletion
MX2015009773A (en) 2013-01-29 2016-08-05 Aptinyx Inc Spiro-lactam nmda receptor modulators and uses thereof.
TR201817995T4 (en) 2013-03-13 2019-02-21 Sage Therapeutics Inc NEUROACTIVE STEROIDS AND METHODS OF USE
MX2015012437A (en) 2013-03-13 2016-04-15 Sage Therapeutics Inc Neuroactive steroids, compositions, and uses thereof.
ES2873248T3 (en) 2014-02-08 2021-11-03 Hoffmann La Roche Methods to treat Alzheimer's disease
EP4306114A1 (en) 2014-06-18 2024-01-17 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
EP3166613A4 (en) 2014-07-09 2018-02-21 Duke University Compositions and methods for the repair of myelin
PE20170907A1 (en) 2014-10-07 2017-07-12 Sage Therapeutics Inc NEUROACTIVE COMPOUNDS AND METHODS OF USING THEM
IL282048B2 (en) 2015-07-06 2024-09-01 Sage Therapeutics Inc Oxysterols and methods of use thereof
KR20240137111A (en) 2015-07-06 2024-09-19 세이지 테라퓨틱스, 인크. Oxysterols and methods of use thereof
CA2991311A1 (en) 2015-07-06 2017-01-12 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
GB2557875A (en) 2015-09-02 2018-07-04 Univ Swansea Diagnostic methods and kits
CN109195604B (en) 2016-04-01 2023-11-14 萨奇治疗股份有限公司 Oxysterol and methods of use thereof
WO2017193046A1 (en) 2016-05-06 2017-11-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
MD3481846T2 (en) 2016-07-07 2021-11-30 Sage Therapeutics Inc 11-substituted 24-hydroxysterols for use in the treatment of NMDA related conditions
US20190233465A1 (en) 2016-07-11 2019-08-01 Sage Therapeutics, Inc. C7, c12, and c16 substituted neuroactive steroids and their methods of use
CN110023323A (en) 2016-09-30 2019-07-16 萨奇治疗股份有限公司 The oxygen sterol that C7 replaces and its method as NMDA regulator
BR112019008069A2 (en) 2016-10-18 2019-09-03 Sage Therapeutics Inc oxyesterols and methods of use thereof
ES2952106T3 (en) 2016-10-18 2023-10-27 Sage Therapeutics Inc Oxysterols and procedures for their use
WO2018170336A1 (en) 2017-03-15 2018-09-20 Modernatx, Inc. Lipid nanoparticle formulation
KR20200020877A (en) 2017-06-23 2020-02-26 인터셉트 파마슈티컬즈, 인크. Methods and intermediates for the preparation of bile acid derivatives
KR20200085837A (en) 2017-11-10 2020-07-15 마리누스 파마슈티컬스 인코포레이티드 Use of ganasolone for use in the treatment of genetic epilepsy
US20220332699A1 (en) 2019-05-24 2022-10-20 Sage Therapeutics, Inc. Compounds, compositions, and methods of use

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3079385A (en) * 1961-01-24 1963-02-26 Roussel Uclaf Novel process of preparation of polyhydroxylated pregnanes
JPH08268917A (en) * 1995-03-31 1996-10-15 D D S Kenkyusho:Kk Antitumor agent having high transition to cancer tissue
FR2850023A1 (en) * 2003-01-17 2004-07-23 Mapreg Treating acute lesions or degenerative diseases of the nervous system, e.g. Alzheimer's disease, spinal-cerebral trauma or pain, using 3-methoxypregnenolone or derivatives having microtubule stabilizing action

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
CONNICK ET AL.: "Program No. 613 1/B86", 2009 NEUROSCIENCE MEETING PLANNER. CHICAGO, IL: SOCIETY FOR NEUROSCIENCE, 2009, XP002686783 *
CROSS A D ET AL: "Steroids CCLXXIN<1>. Biologically-active labile ethers IV<2>. The synthesis of 22-oxa-25-azacholesterol and related compounds", STEROIDS, ELSEVIER SCIENCE PUBLISHERS, NEW YORK, NY, US, vol. 5, no. 5, 1 May 1965 (1965-05-01), pages 585 - 598, XP023431635, ISSN: 0039-128X, [retrieved on 19650501], DOI: 10.1016/0039-128X(65)90154-6 *
KHRIPACH V A ET AL: "Synthesis of (24S)-hydroxy-and (24S)-24,25-epoxycholesterol analogues, potential agonists of nuclear LXR receptors", RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY, KLUWER ACADEMIC PUBLISHERS-PLENUM PUBLISHERS, NE, vol. 32, no. 6, 1 December 2006 (2006-12-01), pages 586 - 594, XP019453952, ISSN: 1573-9163, DOI: 10.1134/S1068162006060124 *
LARRY K. STEINRAUF ET AL: "Synthesis and evaluation of sulfur-containing steroids against methylmercuric chloride toxicity", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 67, no. 12, 1 December 1978 (1978-12-01), pages 1739 - 1743, XP055043400, ISSN: 0022-3549, DOI: 10.1002/jps.2600671228 *
NAGANO H ET AL: "CHEMISTRY AND BIOCHEMISTRY OF CHINESE DRUGS. PART II. HYDROXYLATED STEROLS, CYTOTOXIC TOWARDS CANCEROUS CELLS: SYNTHESIS AND TESTING", JOURNAL OF CHEMICAL RESEARCH, SCIENCE REVIEWS LTD, GB, vol. 9, 1 January 1977 (1977-01-01), pages 218, XP009025681, ISSN: 0308-2342 *

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